Tolcapone
TASMAR
What it isCentral and peripheral catechol-O-methyltransferase inhibitor used with levodopa/carbidopa for Parkinson disease with motor fluctuations.
Why this oneCrosses the blood-brain barrier and extends levodopa effect more strongly than peripheral-only COMT inhibitors.
What limits itReserved for patients who fail or cannot use other adjuncts; monitor liver tests and stop within 3 weeks if there is no substantial benefit.
FDA-approved for
- Parkinson disease with motor fluctuations (1998)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Parkinson's disease (adjunct to levodopa/carbidopa) | Adult | 100 mg TID | 100 mg TID | 200 mg TID |
Renal Undefined
Hepatic Contraindicated in liver disease; do not initiate if ALT/AST >2x ULN
Instructions
- Only prescribe with concomitant carbidopa/levodopa.
- Withdraw if no substantial clinical benefit within 3 weeks.
- Do not retreat patients withdrawn for hepatocellular injury.
Contraindications
- Liver disease
- Prior tolcapone-induced hepatocellular injury (withdrawn from drug)
- History of nontraumatic rhabdomyolysis or hyperpyrexia and confusion possibly medication-related
Cautions
- Hepatocellular injury / fulminant liver failure - monitor LFTs
- Rhabdomyolysis
- Use caution with severe dyskinesia or dystonia
- Events reported with dopaminergic therapy (hallucinations, hypotension)
Adverse reactions
- Severe hepatocellular injury incl. fatal fulminant liver failure
- Elevated ALT/AST
Pregnancy No adequate human data; animal embryo-fetal toxicity; given with levodopa/carbidopa (teratogenic in rabbits)
Lactation Undefined
⚠ BOXED WARNINGS
- Potentially fatal acute fulminant liver failure
- Use only for levodopa-treated Parkinson disease with fluctuations not adequately managed by other adjuncts
- Stop if substantial benefit is absent within 3 weeks
Cost, est. cash$10–$500/month
Generic entry2015
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityOrthostasis, hallucinations, dyskinesia and impulse-control symptoms; abrupt withdrawal can be hazardous.
Mechanism of action: Tolcapone ballicule
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Memory aids: mascots and interaction avatars
